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M&R > ANS drugs > Flashcards

ANS drugs Flashcards

0
Q

What is acetylcholine degraded to? (By acetylcholine esterase)

A

Choline and acetate

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1
Q

How is acetyl choline synthesised? Where?

A 
Choline acetyltransferase (CAT) catalyses the reaction of choline and acetyl CoA 
In the cytoplasm of cholinergic terminals
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2
Q

At which type of cholinergic synapse is the activity of acetyl cholinesterase the highest at?

A

Fast (nicotinic) cholinergic synapses

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3
Q

How is noradrenaline synthesised?

A

Within the nerve terminal
Tyrosine ➡️ dopa (tyrosine hydroxylase) (rate limiting step)
Dopa ➡️ dopamine

In synaptic vesicles
Dopamine ➡️ noradrenaline (dopamine β-hydroxylase)

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4
Q

Why can noradrenaline be recycled?

A

The vesicular transporter recognises noradrenaline as well as dopamine.

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5
Q

How is the intra-vesicular concentration of noradrenaline kept high?

A

H+-ATPase generates a cytoplasm-vesicle H+ gradient to move catecholamines against their concentration gradient.

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6
Q

What is cytoplasmic noradrenaline broken down by?

A

Monoamine oxidase

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7
Q

What removes noradrenaline from the synaptic cleft?

A

High affinity reuptake system - uptake 1

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8
Q

What are the major drug classes acting on cholinergic nerve terminals?

A

Nicotinic cholinoceptor antagonists
Muscarinic cholinoceptor agonists and antagonists
Cholinesterase inhibitors

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9
Q

Example of a nicotinic cholinoceptor antagonist and its action?

A

Tubocurarine

Muscle paralysis during anaesthesia

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10
Q

Example of a muscarinic cholinoceptor antagonist? Action?

A

Ipratropium bromide

Treat bronchoconstriction in asthmatics

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11
Q

Example of a cholinesterase inhibitor and its action?

A

Endrophonium

Treatment of glaucoma or myasthenia gravis

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12
Q

Classes of drugs acting on adrenergic receptors?

A

Selective β1, β2 and α1 agonists
Selective α1 and α2 antagonists
β antagonists (blockers)

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13
Q

Example of a selective β1 agonists and its action?

A

Dobutamine

Positive inotropic/chronotropic effects in the heart

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14
Q

Example of selective β2 agonist and its effect?

A

Salbutamol

Bronchodilation

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15
Q

Example of a selective α1 agonist and its action?

A

Adrenaline

Vasoconstriction to retard dissipation of anaesthetic

16
Q

Selective α2 agonist and its action?

A

Clonidine
Anti hypertension
Acts on presynaptic receptors to reduce NA release

17
Q

Example of an α-antagonist and its effect?

A

Phentolamine

Peripheral vasodilation to treat peripheral vascular disease

18
Q

Example of an α1 antagonist and its effect?

A

Prazosin

Hypertension

19
Q

Example of a β antagonist and its effect?

A 
Propranolol
Hypertension
MI
Angina
Unwanted side effect: bronchoconstriction
20
Q

What does α-methyl-tyrosine do?

A

Competitively inhibits tyrosine hydroxylase and therefore blocks de novo synthesis of noradrenaline. Used to inhibits NA synthesis in pheochromocytoma

21
Q

What does α-methyl-DOPA do?

A

Taken up by neurones and converted to α-methyl-noradrenaline. Is it poorly metabolised and therefore accumulates in synaptic vesicles of noradrenergic terminals.
When released by Ca mediated exocytosis, it preferentially activates pre-synaptic α2 receptors.
The βγ subunit of the α2 receptor inhibits the VOCC, reducing Ca mediated neurotransmitter release.

22
Q

What does carbiDOPA do?

A

Inhibits DOPA decarboxylase in the periphery but not in the CNS as it cannot cross the BBB. Used in combination of L-DOPA in treatment of Parkinson’s disease.

23
Q

Effect of adrenergic blocking drugs?

A

Local anaesthetic by reducing impulse conduction, calcium mediated exocytosis and repletion of NA from synaptic vesicles

24
Q

What do indirectly-acting sympathomimetic agents do?

A

Recognised and transported into the adrenergic terminal by uptake 1
Taken into synaptic vesicles
NA is displaces and leaks into synaptic cleft without calcium
Extent to which NA leaks out can be enhanced by inhibition of MAO

25
Q

What class of drugs are tricyclic antidepressants?

A

Uptake 1 inhibitors

26
Q

What are some side effects of the peripheral actions of uptake 1 inhibitors?

A

Tachycardia

Cardiac dysthymias

27
Q

Which type of muscarinic receptor is found in the GI tract?

A

M1

28
Q

Which type of muscarinic receptor is found in the SA node?

A

M2

29
Q

What type of drug can be used to stimulate bladder emptying?

A

Muscarinic cholinoceptor agonist

30
Q

What type of drug can be used to increase GI activity?

A

Muscarinic cholinoceptor agonist

31
Q

Which receptor leads to relaxation of the bladder smooth muscle?

A

β2

M&R (10 decks)

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